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公开(公告)号：US20230241241A1
公开(公告)日：2023-08-03
申请号：US18001899
申请日：2020-06-19
发明人： Robert ZHAO , Qingliang YANG , Hangbo YE , Yuanyuan HUANG , Yifang XU , Gengxiang ZHAO , Diancheng CHEN , Huihui GUO , Xiangfei KONG , Wenjun LI , Lu BAI , Xiang CAI , Xiuzhen ZHANG , Junxiang JIA , Zhixiang GUO , Shangma HUANG , Xiaoxu WANG , Jun ZHENG , Yong DU , Yanhua LI , Yunxia ZHENG , Chen LIN , Xiaoxiao CHEN , Wei ZHENG , Xinyan JIANG , Lingli ZHANG , Riping YE , Miaomiao CHEN
CPC分类号： A61K47/6849 , A61K47/6803 , A61P35/00 , A61K47/6851
摘要： This invention relates to conjugates of camptothecin analogs with a cell-binding molecule of formula (I), wherein R1, R2, R3, R4, R5, X, L, n, m, T and ----- are defined herein. It also provides methods of making the conjugates of camptothecin analogs to a cell-binding agent, as well as methods of using the conjugates in targeted treatment of cancer, infection, and immunological disorders.
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公开(公告)号：US20220323602A1
公开(公告)日：2022-10-13
申请号：US17835041
申请日：2022-06-08
发明人： Yongxin Robert ZHAO , Qingliang YANG , Yuanyuan HUANG , Shun GAI , Hangbo YE , Linyao ZHAO , Chengyu YANG , Huihui GUO , Xiaomai ZHOU , Hongsheng XIE , Haifeng ZHU , Yifang XU , Qianqian TONG , Junxiang JIA , Minjun CAO , Wenjun LI , Shuihong GAO , Zhixiang GUO , Lu BAI , Chen LI , Yanlei YANG , Chunyan WANG , Zhichang YE
IPC分类号： A61K47/68
摘要： The present invention relates to linkers having a group of propiolyl, substituted acryl (acryloyl), or disubstituted propanoyl, and using such linkers for the conjugation of compounds, in particular, cytotoxic agents to a cell-binding molecule.
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公开(公告)号：US20200069814A1
公开(公告)日：2020-03-05
申请号：US16488764
申请日：2017-04-06
发明人： Robert Yongxin ZHAO , Yuanyuan HUANG , Qingliang YANG , Shun GAI , Hangbo YE , Linyao ZHAO , Chengyu YANG , Yifang XU , Huihui GUO , Minjun CHAO , Qianqian TONG , Wenjun LI , Xiang CAI , Xiaomai ZHOU , Hongsheng XIE , Junxiang JIA , Haifeng ZHU , Zhixiang GUO , Shuihong GAO , Chunyan WANG , Chen LIN , Yanlei YANG , Zhicang YE , Jie PENG , Jun XU , Xiaotao ZUO , Qingyu SU
IPC分类号： A61K47/68
摘要： A conjugation of a cytotoxic drug to a cell-binding molecule with a bis-linker (dual-linker) as shown in Formula (I). Bis-linkage methods of making a conjugate of a cytotoxic drug/molecule to a cell-binding agent in a specific manner are also described, as well as application of the conjugates for the treatment of a cancer, or an autoimmune disease, or an infectious disease. wherein “” is an optional bond; X, Y, Z1, and Z2 are a functional group; m1 and n are a integer; L1 and L2 are a linker.
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公开(公告)号：US20230115871A1
公开(公告)日：2023-04-13
申请号：US17622360
申请日：2019-06-24
发明人： Robert Yongxin ZHAO , Qingliang YANG , Linyao ZHAO , Yuanyuan HUANG , Hangbo YE , Shun GAI , Junxiang JIA , Lu BAI , Wenjun LI , Zhixiang GUO , Chen LIN , Jun ZHENG , Huihui GUO , Minjun CAO , Xiangfei KONG , Yong DU , Yifang XU , Xiaomai ZHOU , Hongsheng XIE , Xiuzhen ZHANG , Miaomiao CHEN , Xiaolei LIU , Xiang CAI , Binbin CHEN , Yanlei YANG , Lingli ZHANG
IPC分类号： A61K47/68
摘要： The present invention relates to the conjugation of cytotoxic drug to a cell-binding molecule with a side-chain linker. It provides side-chain linkage methods of making a conjugate of a cytotoxic molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and immunological disorders.
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公开(公告)号：US20230057350A1
公开(公告)日：2023-02-23
申请号：US17426813
申请日：2019-01-31
发明人： Robert Yongxin ZHAO , Qingliang YANG , Jun LEI , Yuanyuan HUANG , Linyao ZHAO , Hangbo YE , Shun GAI , Mingjun CAO , Qianqian TONG , Lu BAI , Zhixiang GUO , Chengyu YANG , Xiaomai ZHOU , Hongsheng XIE , Yifang XU , Huihui GUO , Junxiang JIA , Jun ZHENG , Cheng LIN , Xiaotao ZHUO , Wenjun LI , Yong DU , Xiangfei KONG , Binbin CHEN , Yanlei YANG , Yanhong TONG , Xiaoxiao CHEN , Yanhua LI , Xiuzheng ZHANG , Juan LAI
摘要： Provided herein is the conjugation of an amanita toxin compound to a cell-binding molecule with branched linkers for having better targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of an amanita molecule to a cell-binding ligand, as well as methods of using the conjugate in targets treatment of cancer, infection and autoimmune disease.
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公开(公告)号：US20220313836A1
公开(公告)日：2022-10-06
申请号：US17835081
申请日：2022-06-08
发明人： Yongxin Robert ZHAO , Qingliang YANG , Yuanyuan HUANG , Shun GAI , Hangbo YE , Linyao ZHAO , Chengyu YANG , Huihui GUO , Xiaomai ZHOU , Hongsheng XIE , Haifeng ZHU , Yifang XU , Qianqian TONG , Junxiang JIA , Minjun CAO , Wenjun LI , Shuihong GAO , Zhixiang GUO , Lu BAI , Chen LI , Yanlei YANG , Chunyan WANG , Zhichang YE
IPC分类号： A61K47/68
摘要： The present invention relates to linkers having a group of propiolyl, substituted acryl (acryloyl), or disubstituted propanoyl, and using such linkers for the conjugation of compounds, in particular, cytotoxic agents to a cell-binding molecule.
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公开(公告)号：US20200276261A1
公开(公告)日：2020-09-03
申请号：US16759175
申请日：2017-12-31
发明人： Robert Yongxin ZHAO , Qingliang YANG , Yuanyuan HUANG , Linyao ZHAO , Shun GAI , Hangbo YE , Jun LEI , Yifang XU , Mingjun CAO , Huihui GUO , Junxiang JIA , Qianqian TONG , Wenjun LI , Xiaomai ZHOU , Hongsheng XIE , Lu BAI , Xiang CAI , Xiaotao ZHUO , Xiuzheng ZHANG , Jun ZHENG
摘要： The present invention relates to the conjugation of a tubulysin analog compound to a cell-binding molecule with branched/side-chain linkers for having better delivery of the conjugate compound and targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of a tubulysin analog molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and autoimmune disease.
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公开(公告)号：US20230165930A1
公开(公告)日：2023-06-01
申请号：US18156709
申请日：2023-01-19
发明人： Robert Yongxin ZHAO , Qingliang YANG , Yuanyuan HUANG , Linyao ZHAO , Shun GAI , Hangbo YE , Jun LEI , Yifang XU , Mingjun CAO , Huihui GUO , Junxiang JIA , Qianqian TONG , Wenjun LI , Xiaomai ZHOU , Hongsheng XIE , Lu BAI , Xiang CAI , Xiaotao ZHUO , Xiuzheng ZHANG , Jun ZHENG
CPC分类号： A61K38/07 , A61K45/06 , C07K5/1024
摘要： Described is a conjugation of a tubulysin analog compound to a cell-binding molecule with branched/side-chain linkers for having better delivery of the conjugate compound and targeted treatment of abnormal cells. Also described are a branched-linkage method of conjugation of a tubulysin analog molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and autoimmune disease.
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公开(公告)号：US20230149502A1
公开(公告)日：2023-05-18
申请号：US18156793
申请日：2023-01-19
发明人： Robert Yongxin ZHAO , Qingliang YANG , Yuanyuan HUANG , Linyao ZHAO , Shun GAI , Hangbo YE , Jun LEI , Yifang XU , Mingjun CAO , Huihui GUO , Junxiang JIA , Qianqian TONG , Wenjun LI , Xiaomai ZHOU , Hongsheng XIE , Lu BAI , Xiang CAI , Xiaotao ZHUO , Xiuzheng ZHANG , Jun ZHENG
CPC分类号： A61K38/07 , A61K45/06 , C07K5/1024
摘要： Described is a conjugation of a tubulysin analog compound to a cell-binding molecule with branched/side-chain linkers for having better delivery of the conjugate compound and targeted treatment of abnormal cells. Also described are a branched-linkage method of conjugation of a tubulysin analog molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and autoimmune disease.
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公开(公告)号：US20220249594A1
公开(公告)日：2022-08-11
申请号：US17596956
申请日：2020-02-18
发明人： Robert ZHAO , Qingliang YANG , Yuanyuan HUANG , Shun GAI , Hangbo YE , Linyao ZHAO , Huihui GUO , Lu BAI , Wenjun LI , Junxiang JIA , Zhixiang GUO , Jun ZHENG , Xiaoxiao CHEN , Xiangfei KONG , Chen LIN , Yong DU , Yu ZHANG , Lei ZHOU , Xiuzhen ZHANG , Xiuhong ZHENG , Binbin CHEN , Yanlei YANG , Meng DAI , Yifang XU , Zhongliang FAN , Xiaomai ZHOU , Xingyan JIANG , Miaomiao CHEN , Lingli ZHANG , Yanhua LI
摘要： A formulation of conjugates of tubulysin analogs with a cell-binding molecule having a structure represented by Formula (I), wherein T, L, m, n, ----, R1, R2, R3, R4, R1, R6, R7, R1, R9, R10, R11, R12, and R13 are as defined herein, can be used for targeted treatment of cancer, autoimmune disease, and infectious disease.
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